|Systematic (IUPAC) name|
|Mol. mass||281.42 g/mol|
Xanomeline (LY-246,708; Lumeron, Memcor) is a muscarinic acetylcholine receptor agonist with reasonable selectivity for the M1 and M4 subtypes, though it is also known to act as a M5 receptor antagonist. It has been studied for the treatment of both Alzheimer's disease and schizophrenia, particularly the cognitive and negative symptoms, although gastrointestinal side effects led to a high drop-out rate in clinical trials. Despite this, xanomeline has been shown to have reasonable efficacy for the treatment of schizophrenia symptoms, and one recent human study found robust improvements in verbal learning and short-term memory associated with xanomeline treatment.
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- Woolley ML, Carter HJ, Gartlon JE, Watson JM, Dawson LA (January 2009). "Attenuation of amphetamine-induced activity by the non-selective muscarinic receptor agonist, xanomeline, is absent in muscarinic M4 receptor knockout mice and attenuated in muscarinic M1 receptor knockout mice". European Journal of Pharmacology 603 (1-3): 147–9.
- Heinrich JN, Butera JA, Carrick T, et al. (March 2009). "Pharmacological comparison of muscarinic ligands: historical versus more recent muscarinic M1-preferring receptor agonists". European Journal of Pharmacology 605 (1-3): 53–6.
- Grant MK, El-Fakahany EE (October 2005). "Persistent binding and functional antagonism by xanomeline at the muscarinic M5 receptor". The Journal of Pharmacology and Experimental Therapeutics 315 (1): 313–9.
- Lieberman JA, Javitch JA, Moore H (August 2008). "Cholinergic agonists as novel treatments for schizophrenia: the promise of rational drug development for psychiatry". The American Journal of Psychiatry 165 (8): 931–6.
- Messer WS (2002). "The utility of muscarinic agonists in the treatment of Alzheimer's disease". Journal of Molecular Neuroscience : MN 19 (1-2): 187–93.
- Mirza NR, Peters D, Sparks RG (2003). "Xanomeline and the antipsychotic potential of muscarinic receptor subtype selective agonists". CNS Drug Reviews 9 (2): 159–86.
- Shekhar A, Potter WZ, Lightfoot J, et al. (August 2008). "Selective muscarinic receptor agonist xanomeline as a novel treatment approach for schizophrenia". The American Journal of Psychiatry 165 (8): 1033–9.